Nimesulide is a relatively COX-2 selective, non-steroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic properties. Its approved indications are the treatment of acute pain, the symptomatic treatment of osteoarthritis and primary dysmenorrhoea in adolescents and adults above 12 years old. Due to concerns about the risk of hepatotoxicity, nimesulide has been withdrawn from market in many countries.

Pharmacodynamics

Pharmacokinetics

Nimesulide is a nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory, anti-pyretic, and analgesic properties. It inhibits prostaglandin synthetase/cyclooxygenase, which limits prostaglandin production. Its cyclooxygenase inhibiting potency is intermediate, but is relatively selective for the cyclo-oxygenase-2 (COX-2) thus the potential for gastric injury and intolerance is less. It is also a free radical scavenger, and helps protect against the tissue damage that occurs during inflammation.AbsorptionWell absorbed from GI tract following oral admin. Peak plasma levels:1-3 hours. With bid admin of 100 mg, steady-state is achieved within 24-36 hours.

Precautions

Special Precautions

Other Drug Interactions

Additive hepatotoxic effects with known hepatotoxins: anti-convulsants (e.g. valproic acid), anti-fungals (e.g. ketoconazole), anti-tuberculous drugs (e.g. isoniazid), tacrine, pemoline, amiodarone, methotrexate, methyldopa, amoxicillin/clavulanic acid. May decrease the oral bioavailability of furosemide and the natriuretic and diuretic response to furosemide. Increased risks of GI and hepatic adverse effects with other NSAIDs, including aspirin. May increase anti-coagulant effect of warfarin. Potentiates the action of phenytoin. May be displaced from binding sites with fenofibrate, salicylic acid, and tolbutamide. Interactions between NSAIDs and lithium, probenecid and ciclosporin, have been documented.

Other Interactions

Food InteractionAlcohol increases the risk of hepatic reactions.

Dosage

OralDysmenorrhoeaAdult: 100 mg bid. Use in the European Union (EU) is limited to a max of 15 days.

OralOsteoarthritisAdult: 100 mg bid. Use in the European Union (EU) is limited to a max of 15 days.OralPostoperative painAdult: 100 mg bid. Use in the European Union (EU) is limited to a max of 15 days.